| 摘要 |
<p>Compounds of formula (I) are modulators of cannabinoid receptor CB1, useful inter alia for treatment of obesity: Formula (I). Wherein: X is a bond, or a divalent radical selected from—C(R10)(R11)—*,—C(R10)(R11)—O—*,—C(R10)(R11)CH2—*,—C(R10)(R11)CH2—O—*,—CH2C(R10)(R11)—*,—CH2C(R10)(R11)—O—*, and—CH2—O—C(R10)(R11)—*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; Z is a carboxyl isostere radical selected from the group specified; R3 is hydrogen, (C1-C)alkyl or (C1C3)fluoroalkyl; R4 is a radical of formula -(Alk1)p-(Q1)r (L)s-Q2 wherein p, r, s, Alk1, L, Q1 and Q2 are as specified; or R3and R4 taken together with the nitrogen to which they are attached form a cyclic amino ring of 4 to 7 ring atoms which is optionally substituted by a radical of formula -(L)s-Q2 wherein s, L and Q2 are as defined above, or by an optional substituent selected from hydroxy, methoxy,—NH2—, or mono- or di-(C1C3)alkylamino; R5, R6, R7 and R8 are each independently selected from hydrogen—F,—Cl,—Br,—CN, (C1-C3)alkyl, (C1C3)fluoroalkyl, cyclopropyl, and—OR9; R10 is hydrogen, (C1C3)alkyl, hydroxyl or NH2, and R11 is hydrogen or (C1-C3)alkyl; or R10 and R11 taken together with the carbon atom to which they are attached form a (C3-C5)cycloalkyl ring.</p> |
